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Items: 1 to 50 of 54

1.

Quantitative structural assessment of graded receptor agonism.

Shang J, Brust R, Griffin PR, Kamenecka TM, Kojetin DJ.

Proc Natl Acad Sci U S A. 2019 Oct 29;116(44):22179-22188. doi: 10.1073/pnas.1909016116. Epub 2019 Oct 14.

PMID:
31611383
2.

The Tat inhibitor didehydro-cortistatin A suppresses SIV replication and reactivation.

Mediouni S, Kessing CF, Jablonski JA, Thenin-Houssier S, Clementz M, Kovach MD, Mousseau G, de Vera IMS, Li C, Kojetin DJ, Evans DT, Valente ST.

FASEB J. 2019 Jul;33(7):8280-8293. doi: 10.1096/fj.201801165R. Epub 2019 Apr 25.

PMID:
31021670
3.

Structural Basis of Altered Potency and Efficacy Displayed by a Major in Vivo Metabolite of the Antidiabetic PPARγ Drug Pioglitazone.

Mosure SA, Shang J, Eberhardt J, Brust R, Zheng J, Griffin PR, Forli S, Kojetin DJ.

J Med Chem. 2019 Feb 28;62(4):2008-2023. doi: 10.1021/acs.jmedchem.8b01573. Epub 2019 Feb 7.

PMID:
30676741
4.

REV-ERBα Regulates TH17 Cell Development and Autoimmunity.

Amir M, Chaudhari S, Wang R, Campbell S, Mosure SA, Chopp LB, Lu Q, Shang J, Pelletier OB, He Y, Doebelin C, Cameron MD, Kojetin DJ, Kamenecka TM, Solt LA.

Cell Rep. 2018 Dec 26;25(13):3733-3749.e8. doi: 10.1016/j.celrep.2018.11.101.

5.

Cooperative cobinding of synthetic and natural ligands to the nuclear receptor PPARγ.

Shang J, Brust R, Mosure SA, Bass J, Munoz-Tello P, Lin H, Hughes TS, Tang M, Ge Q, Kamenekca TM, Kojetin DJ.

Elife. 2018 Dec 21;7. pii: e43320. doi: 10.7554/eLife.43320.

6.

Structural organization of a major neuronal G protein regulator, the RGS7-Gβ5-R7BP complex.

Patil DN, Rangarajan ES, Novick SJ, Pascal BD, Kojetin DJ, Griffin PR, Izard T, Martemyanov KA.

Elife. 2018 Dec 12;7. pii: e42150. doi: 10.7554/eLife.42150.

7.

Defining a Canonical Ligand-Binding Pocket in the Orphan Nuclear Receptor Nurr1.

de Vera IMS, Munoz-Tello P, Zheng J, Dharmarajan V, Marciano DP, Matta-Camacho E, Giri PK, Shang J, Hughes TS, Rance M, Griffin PR, Kojetin DJ.

Structure. 2019 Jan 2;27(1):66-77.e5. doi: 10.1016/j.str.2018.10.002. Epub 2018 Nov 8.

PMID:
30416039
8.

A structural mechanism for directing corepressor-selective inverse agonism of PPARγ.

Brust R, Shang J, Fuhrmann J, Mosure SA, Bass J, Cano A, Heidari Z, Chrisman IM, Nemetchek MD, Blayo AL, Griffin PR, Kamenecka TM, Hughes TS, Kojetin DJ.

Nat Commun. 2018 Nov 8;9(1):4687. doi: 10.1038/s41467-018-07133-w.

9.

Chemical Crosslinking Mass Spectrometry Reveals the Conformational Landscape of the Activation Helix of PPARγ; a Model for Ligand-Dependent Antagonism.

Zheng J, Corzo C, Chang MR, Shang J, Lam VQ, Brust R, Blayo AL, Bruning JB, Kamenecka TM, Kojetin DJ, Griffin PR.

Structure. 2018 Nov 6;26(11):1431-1439.e6. doi: 10.1016/j.str.2018.07.007. Epub 2018 Aug 23.

10.

Defining a conformational ensemble that directs activation of PPARγ.

Chrisman IM, Nemetchek MD, de Vera IMS, Shang J, Heidari Z, Long Y, Reyes-Caballero H, Galindo-Murillo R, Cheatham TE 3rd, Blayo AL, Shin Y, Fuhrmann J, Griffin PR, Kamenecka TM, Kojetin DJ, Hughes TS.

Nat Commun. 2018 May 4;9(1):1794. doi: 10.1038/s41467-018-04176-x.

11.

Cryptic glucocorticoid receptor-binding sites pervade genomic NF-κB response elements.

Hudson WH, Vera IMS, Nwachukwu JC, Weikum ER, Herbst AG, Yang Q, Bain DL, Nettles KW, Kojetin DJ, Ortlund EA.

Nat Commun. 2018 Apr 6;9(1):1337. doi: 10.1038/s41467-018-03780-1.

12.

Synergistic Regulation of Coregulator/Nuclear Receptor Interaction by Ligand and DNA.

de Vera IMS, Zheng J, Novick S, Shang J, Hughes TS, Brust R, Munoz-Tello P, Gardner WJ Jr, Marciano DP, Kong X, Griffin PR, Kojetin DJ.

Structure. 2017 Oct 3;25(10):1506-1518.e4. doi: 10.1016/j.str.2017.07.019. Epub 2017 Sep 7.

13.

Tethering not required: the glucocorticoid receptor binds directly to activator protein-1 recognition motifs to repress inflammatory genes.

Weikum ER, de Vera IMS, Nwachukwu JC, Hudson WH, Nettles KW, Kojetin DJ, Ortlund EA.

Nucleic Acids Res. 2017 Aug 21;45(14):8596-8608. doi: 10.1093/nar/gkx509.

14.

Modification of the Orthosteric PPARγ Covalent Antagonist Scaffold Yields an Improved Dual-Site Allosteric Inhibitor.

Brust R, Lin H, Fuhrmann J, Asteian A, Kamenecka TM, Kojetin DJ.

ACS Chem Biol. 2017 Apr 21;12(4):969-978. doi: 10.1021/acschembio.6b01015. Epub 2017 Feb 16.

15.

Systems Structural Biology Analysis of Ligand Effects on ERα Predicts Cellular Response to Environmental Estrogens and Anti-hormone Therapies.

Nwachukwu JC, Srinivasan S, Bruno NE, Nowak J, Wright NJ, Minutolo F, Rangarajan ES, Izard T, Yao XQ, Grant BJ, Kojetin DJ, Elemento O, Katzenellenbogen JA, Nettles KW.

Cell Chem Biol. 2017 Jan 19;24(1):35-45. doi: 10.1016/j.chembiol.2016.11.014. Epub 2016 Dec 29.

16.

Probing the Complex Binding Modes of the PPARγ Partial Agonist 2-Chloro-N-(3-chloro-4-((5-chlorobenzo[d]thiazol-2-yl)thio)phenyl)-4-(trifluoromethyl)benzenesulfonamide (T2384) to Orthosteric and Allosteric Sites with NMR Spectroscopy.

Hughes TS, Shang J, Brust R, de Vera IMS, Fuhrmann J, Ruiz C, Cameron MD, Kamenecka TM, Kojetin DJ.

J Med Chem. 2016 Nov 23;59(22):10335-10341. doi: 10.1021/acs.jmedchem.6b01340. Epub 2016 Nov 4.

17.

Activity-Based Profiling Reveals a Regulatory Link between Oxidative Stress and Protein Arginine Phosphorylation.

Fuhrmann J, Subramanian V, Kojetin DJ, Thompson PR.

Cell Chem Biol. 2016 Aug 18;23(8):967-977. doi: 10.1016/j.chembiol.2016.07.008. Epub 2016 Aug 11.

18.

Mechanistic insight into protein modification and sulfur mobilization activities of noncanonical E1 and associated ubiquitin-like proteins of Archaea.

Hepowit NL, de Vera IM, Cao S, Fu X, Wu Y, Uthandi S, Chavarria NE, Englert M, Su D, Sӧll D, Kojetin DJ, Maupin-Furlow JA.

FEBS J. 2016 Oct;283(19):3567-3586. doi: 10.1111/febs.13819.

19.

Identification of a Binding Site for Unsaturated Fatty Acids in the Orphan Nuclear Receptor Nurr1.

de Vera IM, Giri PK, Munoz-Tello P, Brust R, Fuhrmann J, Matta-Camacho E, Shang J, Campbell S, Wilson HD, Granados J, Gardner WJ Jr, Creamer TP, Solt LA, Kojetin DJ.

ACS Chem Biol. 2016 Jul 15;11(7):1795-9. doi: 10.1021/acschembio.6b00037. Epub 2016 Apr 29.

20.

Ebselen, a Small-Molecule Capsid Inhibitor of HIV-1 Replication.

Thenin-Houssier S, de Vera IM, Pedro-Rosa L, Brady A, Richard A, Konnick B, Opp S, Buffone C, Fuhrmann J, Kota S, Billack B, Pietka-Ottlik M, Tellinghuisen T, Choe H, Spicer T, Scampavia L, Diaz-Griffero F, Kojetin DJ, Valente ST.

Antimicrob Agents Chemother. 2016 Mar 25;60(4):2195-208. doi: 10.1128/AAC.02574-15. Print 2016 Apr.

21.

Distal substitutions drive divergent DNA specificity among paralogous transcription factors through subdivision of conformational space.

Hudson WH, Kossmann BR, de Vera IM, Chuo SW, Weikum ER, Eick GN, Thornton JW, Ivanov IN, Kojetin DJ, Ortlund EA.

Proc Natl Acad Sci U S A. 2016 Jan 12;113(2):326-31. doi: 10.1073/pnas.1518960113. Epub 2015 Dec 29.

22.

Structural mechanism for signal transduction in RXR nuclear receptor heterodimers.

Kojetin DJ, Matta-Camacho E, Hughes TS, Srinivasan S, Nwachukwu JC, Cavett V, Nowak J, Chalmers MJ, Marciano DP, Kamenecka TM, Shulman AI, Rance M, Griffin PR, Bruning JB, Nettles KW.

Nat Commun. 2015 Aug 20;6:8013. doi: 10.1038/ncomms9013.

23.

Deconvolution of Complex 1D NMR Spectra Using Objective Model Selection.

Hughes TS, Wilson HD, de Vera IM, Kojetin DJ.

PLoS One. 2015 Aug 4;10(8):e0134474. doi: 10.1371/journal.pone.0134474. eCollection 2015.

24.

Pharmacological repression of PPARγ promotes osteogenesis.

Marciano DP, Kuruvilla DS, Boregowda SV, Asteian A, Hughes TS, Garcia-Ordonez R, Corzo CA, Khan TM, Novick SJ, Park H, Kojetin DJ, Phinney DG, Bruning JB, Kamenecka TM, Griffin PR.

Nat Commun. 2015 Jun 12;6:7443. doi: 10.1038/ncomms8443.

25.

Conserved sequence-specific lincRNA-steroid receptor interactions drive transcriptional repression and direct cell fate.

Hudson WH, Pickard MR, de Vera IM, Kuiper EG, Mourtada-Maarabouni M, Conn GL, Kojetin DJ, Williams GT, Ortlund EA.

Nat Commun. 2014 Nov 7;5:5395. doi: 10.1038/ncomms6395.

26.

Structure of REV-ERBβ ligand-binding domain bound to a porphyrin antagonist.

Matta-Camacho E, Banerjee S, Hughes TS, Solt LA, Wang Y, Burris TP, Kojetin DJ.

J Biol Chem. 2014 Jul 18;289(29):20054-66. doi: 10.1074/jbc.M113.545111. Epub 2014 May 28.

27.

Resveratrol modulates the inflammatory response via an estrogen receptor-signal integration network.

Nwachukwu JC, Srinivasan S, Bruno NE, Parent AA, Hughes TS, Pollock JA, Gjyshi O, Cavett V, Nowak J, Garcia-Ordonez RD, Houtman R, Griffin PR, Kojetin DJ, Katzenellenbogen JA, Conkright MD, Nettles KW.

Elife. 2014 Apr 25;3:e02057. doi: 10.7554/eLife.02057.

28.

An alternate binding site for PPARγ ligands.

Hughes TS, Giri PK, de Vera IM, Marciano DP, Kuruvilla DS, Shin Y, Blayo AL, Kamenecka TM, Burris TP, Griffin PR, Kojetin DJ.

Nat Commun. 2014 Apr 7;5:3571. doi: 10.1038/ncomms4571.

29.

REV-ERB and ROR nuclear receptors as drug targets.

Kojetin DJ, Burris TP.

Nat Rev Drug Discov. 2014 Mar;13(3):197-216. doi: 10.1038/nrd4100. Review.

30.

Ligand-binding dynamics rewire cellular signaling via estrogen receptor-α.

Srinivasan S, Nwachukwu JC, Parent AA, Cavett V, Nowak J, Hughes TS, Kojetin DJ, Katzenellenbogen JA, Nettles KW.

Nat Chem Biol. 2013 May;9(5):326-32. doi: 10.1038/nchembio.1214. Epub 2013 Mar 24.

31.

Nuclear receptors and their selective pharmacologic modulators.

Burris TP, Solt LA, Wang Y, Crumbley C, Banerjee S, Griffett K, Lundasen T, Hughes T, Kojetin DJ.

Pharmacol Rev. 2013 Mar 1;65(2):710-78. doi: 10.1124/pr.112.006833. Print 2013 Apr. Review.

PMID:
23457206
32.

Small molecule modulation of nuclear receptor conformational dynamics: implications for function and drug discovery.

Kojetin DJ, Burris TP.

Mol Pharmacol. 2013 Jan;83(1):1-8. doi: 10.1124/mol.112.079285. Epub 2012 Aug 6. Review.

33.

Regulation of p53 stability and apoptosis by a ROR agonist.

Wang Y, Solt LA, Kojetin DJ, Burris TP.

PLoS One. 2012;7(4):e34921. doi: 10.1371/journal.pone.0034921. Epub 2012 Apr 11.

34.

Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.

Solt LA, Wang Y, Banerjee S, Hughes T, Kojetin DJ, Lundasen T, Shin Y, Liu J, Cameron MD, Noel R, Yoo SH, Takahashi JS, Butler AA, Kamenecka TM, Burris TP.

Nature. 2012 Mar 29;485(7396):62-8. doi: 10.1038/nature11030.

35.

Ligand and receptor dynamics contribute to the mechanism of graded PPARγ agonism.

Hughes TS, Chalmers MJ, Novick S, Kuruvilla DS, Chang MR, Kamenecka TM, Rance M, Johnson BA, Burris TP, Griffin PR, Kojetin DJ.

Structure. 2012 Jan 11;20(1):139-50. doi: 10.1016/j.str.2011.10.018.

36.

Structural and biophysical insights into the ligand-free Pitx2 homeodomain and a ring dermoid of the cornea inducing homeodomain mutant.

Doerdelmann T, Kojetin DJ, Baird-Titus JM, Solt LA, Burris TP, Rance M.

Biochemistry. 2012 Jan 17;51(2):665-76. doi: 10.1021/bi201639x. Epub 2012 Jan 6.

37.

¹H, ¹³C and ¹⁵N chemical shift assignments for the human Pitx2 homeodomain in complex with a 22-base hairpin DNA.

Doerdelmann T, Kojetin DJ, Baird-Titus JM, Rance M.

Biomol NMR Assign. 2012 Apr;6(1):79-81. doi: 10.1007/s12104-011-9329-y. Epub 2011 Aug 5.

38.

The REV-ERBs and RORs: molecular links between circadian rhythms and lipid homeostasis.

Solt LA, Kojetin DJ, Burris TP.

Future Med Chem. 2011 Apr;3(5):623-38. doi: 10.4155/fmc.11.9. Review.

39.

DNA binding alters coactivator interaction surfaces of the intact VDR-RXR complex.

Zhang J, Chalmers MJ, Stayrook KR, Burris LL, Wang Y, Busby SA, Pascal BD, Garcia-Ordonez RD, Bruning JB, Istrate MA, Kojetin DJ, Dodge JA, Burris TP, Griffin PR.

Nat Struct Mol Biol. 2011 May;18(5):556-63. doi: 10.1038/nsmb.2046. Epub 2011 Apr 10.

40.

A role for rev-erbα ligands in regulation of adipogenesis.

Kojetin DJ, Burris TP.

Curr Pharm Des. 2011;17(4):320-4. Review.

PMID:
21375499
41.

Observing selected domains in multi-domain proteins via sortase-mediated ligation and NMR spectroscopy.

Refaei MA, Combs A, Kojetin DJ, Cavanagh J, Caperelli C, Rance M, Sapitro J, Tsang P.

J Biomol NMR. 2011 Jan;49(1):3-7. doi: 10.1007/s10858-010-9464-2. Epub 2010 Dec 29.

42.

Identification of SR3335 (ML-176): a synthetic RORα selective inverse agonist.

Kumar N, Kojetin DJ, Solt LA, Kumar KG, Nuhant P, Duckett DR, Cameron MD, Butler AA, Roush WR, Griffin PR, Burris TP.

ACS Chem Biol. 2011 Mar 18;6(3):218-22. doi: 10.1021/cb1002762. Epub 2010 Dec 6.

43.

1H, 13C and 15N chemical shift assignments for the human Pitx2 homeodomain and a R24H homeodomain mutant.

Doerdelmann T, Kojetin DJ, Baird-Titus JM, Rance M.

Biomol NMR Assign. 2011 Apr;5(1):105-7. doi: 10.1007/s12104-010-9278-x. Epub 2010 Nov 4.

44.

Characterization of the core mammalian clock component, NPAS2, as a REV-ERBalpha/RORalpha target gene.

Crumbley C, Wang Y, Kojetin DJ, Burris TP.

J Biol Chem. 2010 Nov 12;285(46):35386-92. doi: 10.1074/jbc.M110.129288. Epub 2010 Sep 3.

45.

Structural and motional contributions of the Bacillus subtilis ClpC N-domain to adaptor protein interactions.

Kojetin DJ, McLaughlin PD, Thompson RJ, Dubnau D, Prepiak P, Rance M, Cavanagh J.

J Mol Biol. 2009 Apr 3;387(3):639-52. doi: 10.1016/j.jmb.2009.01.046. Epub 2009 Jan 30.

46.

Insights into the nature of DNA binding of AbrB-like transcription factors.

Sullivan DM, Bobay BG, Kojetin DJ, Thompson RJ, Rance M, Strauch MA, Cavanagh J.

Structure. 2008 Nov 12;16(11):1702-13. doi: 10.1016/j.str.2008.08.014.

47.

Implications of the binding of tamoxifen to the coactivator recognition site of the estrogen receptor.

Kojetin DJ, Burris TP, Jensen EV, Khan SA.

Endocr Relat Cancer. 2008 Dec;15(4):851-70. doi: 10.1677/ERC-07-0281. Epub 2008 Aug 28. Review.

PMID:
18755852
48.

NMR assignment of the N-terminal repeat domain of Bacillus subtilis ClpC.

Kojetin DJ, McLaughlin PD, Thompson RJ, Venters RA, Rance M, Cavanagh J.

Biomol NMR Assign. 2007 Dec;1(2):163-5. doi: 10.1007/s12104-007-9046-8. Epub 2007 Sep 6.

PMID:
19636855
49.

Classification of response regulators based on their surface properties.

Kojetin DJ, Sullivan DM, Thompson RJ, Cavanagh J.

Methods Enzymol. 2007;422:141-69.

PMID:
17628138
50.

Structure, binding interface and hydrophobic transitions of Ca2+-loaded calbindin-D(28K).

Kojetin DJ, Venters RA, Kordys DR, Thompson RJ, Kumar R, Cavanagh J.

Nat Struct Mol Biol. 2006 Jul;13(7):641-7. Epub 2006 Jun 25.

PMID:
16799559

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